Development and bioevaluation of [99m] Tc[CO][3]-labeled [1-azido-1- deoxy-beta -D-glucopyranoside] complex as a potential tumor-seeking agent

ABSTRACT

The 1,2,3-triazole-containing [1-azido-1-deoxy-beta -D-glucopyranoside] complex was synthesized using click chemistry approach and evaluated its potential as a tumor-seeking agent. In the present study, [99m] Tc-tricarbonyl labeled [1-azido-1-deoxy-beta -D-glucopyranoside] radiotracer [[99m] Tc[CO][3]-BM], [where BM stands for biomolecule, e.g., [1- azido-1-deoxy-beta -D- glucopyranoside]] was synthesized via click chemistry approach and then labeled with technetium- 99m through isolink kit. Radio labeled drug was tested for radiochemical purity and in vitro stability by chromatographic techniques. Normal distribution and tumoral uptake were studied in Swiss Webster mice. Radiochemical purity results show 97.9 +/- 1.5% labeling and its in vitro stability were studied at room temperature up to 5h. The radio labeled drug exhibited 73.6 +/- 1.1% binding with blood proteins. Normal distribution of drug shows prominent uptake in brain while in case of tumor-bearing mice, the uptake was maximum in tumor tissue and negligible amount was shown in brain. The biodistribution was further compared with 2-fluoro-2-deoxy glucose [[18]F-FDG], which was used as a positive control. The data indicate that [99m] Tc-tricarbonyl labeled [1-azido-1-deoxy-beta -D- glucopyranoside] radiotracer might be a feasible candidate with reasonable potential for tumor diagnosis